P-toluene-sulfonyl-oxy substituted pyridines

Abstract

Potent dopamine-β-hydroxylase inhibitors having the Formula: ##STR1## which are useful to inhibit dopamine-β-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-β-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.

What is claimed is: 
     
       1. A compound having the formula: ##STR20## in which: X is hydrogen, halogen, halo C 1-4  alkyl, or any accessible combination thereof of up to three substituents; and W is acetoxy, propionyloxy, butyryloxy, or ##STR21## wherein R is hydrogen or C 1-4  alkyl.   
     
     
       2. A compound of claim 1 that is 3-hydroxy-6-acetoxymethylpyridine 3-p-toluenesulfonate. 
     
     
       3. A compound of claim 1 that is 3-hydroxy-6-hydroxymethylpyridine 3-p-toluenesulfonate. 
     
     
       4. A compound of claim 1 that is 3-hydroxypyridine-6-carboxaldehyde 3-p-toluenesulfonate. 
     
     
       5. A compound of claim 1 that is 1-(3'-hydroxypyridyl-6'-methyl)imidazole-2-thiol 3'-p-toluenesulfonate.